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TOLBUTAMIDE Drug Record

  • Summary
  • Interactions
  • Claims
  • TOLBUTAMIDE chembl:CHEMBL782 Approved

    Alternate Names:

    NSC-87833
    RASTINON
    GLYCONON
    PRAMIDEX
    TOLBUTAMIDE
    ORINASE
    NSC-23813
    N-(SULFONYL-P-METHYLBENZENE)-N'-N-BUTYLUREA
    1-BUTYL-3-(P-METHYLPHENYLSULFONYL)UREA
    1-BUTYL-3-(P-TOLYLSULFONYL)UREA
    3-(P-TOLYL-4-SULFONYL)-1-BUTYLUREA
    N-(P-METHYLBENZENESULFONYL)-N'-BUTYLUREA
    N-N-BUTYL-N'-TOSYLUREA
    1-P-TOLUENESULFONYL-3-BUTYLUREA
    N-BUTYL-N'-P-TOLUENESULFONYLUREA
    1-BUTYL-3-TOSYLUREA
    N-(4-METHYLBENZENESULFONYL)-N'-BUTYLUREA
    N-BUTYL-N'-(4-METHYLPHENYLSULFONYL)UREA
    ORINASE (TN)
    N-BUTYL-N'-(P-TOLYLSULFONYL)UREA
    TOLBUTAMIDUM
    TOLYLSULFONYLBUTYLUREA
    TOLBUTAMIDA
    N-(4-METHYLPHENYLSULFONYL)-N'-BUTYLUREA
    TOLBUTAMIDE SODIUM
    ORINASE®
    chembl:CHEMBL782
    drugbank:01124
    pubchem.compound:5505
    chemidplus:64-77-7
    rxcui:10635

    Drug Info:

    Year of Approval approved before 1982
    Drug Class hypoglycemic agents
    Drug Categories tests for diabetes
    Drug Categories sulfur compounds
    FDA Approval Approved before 1982
    Drug Class small molecule
    Drug Indications Hypoglycemic Agents
    Drug Groups investigational
    Drug Categories alimentary tract and metabolism
    Drug Categories cytochrome p-450 cyp2c18 substrates
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories drugs that are mainly renally excreted
    Drug Categories drugs used in diabetes
    Drug Categories oat1/slc22a6 inhibitors
    Drug Categories sulfonylureas
    (5 More Sources)

    Publications:

    Mizuno et al., 2008, Type 2 diabetes and oral antihyperglycemic drugs., Curr. Med. Chem.
    Liu et al., 1999, ATP-dependent activation of K(Ca) and ROMK-type K(ATP) channels in human submandibular gland ductal cells., J. Biol. Chem.
    Smith et al., 1998, Inhibition of the ATP-sensitive potassium channel from mouse pancreatic beta-cells by surfactants., Br. J. Pharmacol.
    Proks et al., 2001, Interaction of stilbene disulphonates with cloned K(ATP) channels., Br. J. Pharmacol.
    Blaisdell J et al., 2004, Discovery of new potentially defective alleles of human CYP2C9., Pharmacogenetics
    Jones BC et al., 1996, Putative active site template model for cytochrome P4502C9 (tolbutamide hydroxylase)., Drug Metab Dispos
    Kirchheiner J et al., 2002, Impact of CYP2C9 and CYP2C19 polymorphisms on tolbutamide kinetics and the insulin and glucose response in healthy volunteers., Pharmacogenetics
    Dai DP et al., 2015, Identification and Functional Assessment of a New CYP2C9 Allelic Variant CYP2C9*59., Drug Metab Dispos
    Gao N et al., 2016, Gene polymorphisms and contents of cytochrome P450s have only limited effects on metabolic activities in human liver microsomes., Eur J Pharm Sci
    Chen H et al., 2020, An identification and functional evaluation of a novel CYP2C9 variant CYP2C9*62., Chem Biol Interact
    Ibeanu GC et al., 1998, An additional defective allele, CYP2C19*5, contributes to the S-mephenytoin poor metabolizer phenotype in Caucasians., Pharmacogenetics
    Ibeanu GC et al., 1999, A novel transversion in the intron 5 donor splice junction of CYP2C19 and a sequence polymorphism in exon 3 contribute to the poor metabolizer phenotype for the anticonvulsant drug S-mephenytoin., J Pharmacol Exp Ther
  • TOLBUTAMIDE   KCNJ1

    Interaction Score: 2.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10455193 9647478 11226127


    Sources:
    TEND TdgClinicalTrial DrugBank

  • TOLBUTAMIDE   ABCC8

    Interaction Score: 1.49

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker
    Direct Interaction yes

    PMIDs:
    18220763


    Sources:
    TTD DrugBank ChemblInteractions

  • TOLBUTAMIDE   ABCC9

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TOLBUTAMIDE   KCNJ8

    Interaction Score: 0.59

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand None

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TOLBUTAMIDE   KCNJ11

    Interaction Score: 0.44

    Interaction Types & Directionality:
    blocker (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker
    Direct Interaction yes
    Specific Action of the Ligand None

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • TOLBUTAMIDE   G6PD

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA PharmGKB

  • TOLBUTAMIDE   CYP2C9

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15284535 8742240 11875364 25994031 27339126 32531309


    Sources:
    PharmGKB

  • TOLBUTAMIDE   CYP2C19

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10022751 10411572


    Sources:
    PharmGKB

  • DrugBank: DB01124

    • Version: 5.1.7

    Alternate Names:
    Orinase 1gm Drug Brand
    Rastinon Drug Brand
    Tolbutamide Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Mizuno et al., 2008, Type 2 diabetes and oral antihyperglycemic drugs., Curr. Med. Chem.
    Liu et al., 1999, ATP-dependent activation of K(Ca) and ROMK-type K(ATP) channels in human submandibular gland ductal cells., J. Biol. Chem.
    Smith et al., 1998, Inhibition of the ATP-sensitive potassium channel from mouse pancreatic beta-cells by surfactants., Br. J. Pharmacol.

  • TEND: TOLBUTAMIDE

    • Version: 01-August-2011

    Alternate Names:
    TOLBUTAMIDE Primary Drug Name

    Drug Info:
    Drug Class hypoglycemic agents
    Year of Approval approved before 1982

    Publications:

  • TdgClinicalTrial: TOLBUTAMIDE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Hypoglycemic Agents
    Drug Class small molecule
    FDA Approval Approved before 1982

    Publications:

  • PharmGKB: tolbutamide

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Blaisdell J et al., 2004, Discovery of new potentially defective alleles of human CYP2C9., Pharmacogenetics
    Jones BC et al., 1996, Putative active site template model for cytochrome P4502C9 (tolbutamide hydroxylase)., Drug Metab Dispos
    Kirchheiner J et al., 2002, Impact of CYP2C9 and CYP2C19 polymorphisms on tolbutamide kinetics and the insulin and glucose response in healthy volunteers., Pharmacogenetics

  • TTD: Tolbutamide

    • Version: 2020.06.01

    Alternate Names:
    D06OIV TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 178103454

    • Version: 29-September-2020

    Alternate Names:
    TOLBUTAMIDE GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL782

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL782

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Tolbutamide

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

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A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21